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Fluconazole

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Fluconazole is utilized to treat various fungal infections. It acts by interrupting the cell membrane synthesis of the infecting fungi. It is essential to complete the full course of treatment as prescribed, even if symptoms improve, to ensure the infection is cleared effectively.


Ingredient
Category
Availability
In Stock
Delivery
Airmail (14-21 days) | EMS trackable (5-9 days)
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Product Sheet

Active Ingredient(s)
Fluconazole
Reference Brand
Fluconazole
Manufacturer
Pfizer
Product Form
Tablet, Capsule
Regulatory Classification
Rx
Primary Category
Antifungals
Product Category
Triazole antifungal
Pharmacological Class
Azole
Clinical Indications
Yeast infections, Cryptococcal meningitis
Manufacturer Description
Fluconazole is utilized to treat various fungal infections. It acts by interrupting the cell membrane synthesis of the infecting fungi. It is essential to complete the full course of treatment as prescribed, even if symptoms improve, to ensure the infection is cleared effectively.
Mechanism of Action
Fluconazole inhibits the growth of fungi by preventing them from creating their protective cell membranes, effectively stopping the spread of infection.
Route of Administration
Oral
Onset Time
1–2 days
Duration
30–50 hours
Contraindications
Hypersensitivity to azoles
Severe Adverse Events
Liver toxicity, Severe skin reactions, Heart rhythm changes
Common Side Effects
Nausea, Headache, Stomach upset
Uncommon Side Effects
Dizziness, Diarrhea, Rash
Drug Interactions
Warfarin, Rifampicin, Erythromycin
Pregnancy Safety Warnings
Consult with a specialist regarding use during pregnancy.
Storage Guidelines
Store at room temperature, protected from moisture.
Related Products
Itraconazole, Ketoconazole

Fluconazole FAQ

Can fluoro­conazole be taken on an empty stomach?

Yes, fluoro­conazole may be taken with or without food. Some individuals prefer taking it with a meal to lessen occasional stomach upset.

What should I do if I miss a dose of fluoro­conazole?

Take the missed dose as soon as you remember, unless it is almost time for the next scheduled dose. In that case, skip the missed dose and continue with your regular dosing schedule. Do not double the dose.

Is fluoro­conazole safe for people with liver disease?

Fluoro­conazole is metabolized by the liver, so patients with moderate to severe hepatic impairment should use it only under medical supervision, often at reduced doses and with regular liver-function monitoring.

How long does fluoro­conazole stay in the body?

The drug has a long half-life of about 30 hours, allowing once-daily dosing for most infections. Steady-state concentrations are typically reached after 5-7 days of consistent use.

Can fluoro­conazole affect birth control pills?

Fluoro­conazole can increase hormone levels by inhibiting their metabolism, potentially enhancing contraceptive effectiveness. Nonetheless, additional non-hormonal contraception is advised during treatment.

What are the signs of a serious allergic reaction to fluoro­conazole?

Symptoms may include rash, itching, swelling of the face or throat, severe dizziness, or difficulty breathing. Seek emergency medical care immediately if these occur.

Is fluoro­conazole effective against nail fungus?

Oral fluoro­conazole can be used for certain onychomycosis cases, but therapy usually requires higher doses (e.g., 150 mg weekly) for several months and is less common than other agents such as terbinafine.

Can I travel internationally with fluoro­conazole tablets?

Yes, but keep the medication in its original labeled container, bring a copy of the prescription, and be prepared to show it to customs or airline security if requested.

What should I know about fluoro­conazole and alcohol consumption?

While there is no direct chemical interaction, excessive alcohol can increase liver strain. Moderate alcohol intake is generally acceptable, but heavy drinking should be avoided during therapy.

Fluconazole: Generic Medication Overview

Fluconazole belongs to the antifungal class of medications. It is the active ingredient in a range of oral pills that are available in strengths of 50 mg, 100 mg, 150 mg, 200 mg, and 400 mg. In Hong Kong, fluoro­conazole is a prescription-only medicine regulated by the Department of Health. It is commonly prescribed for a variety of fungal infections affecting the skin, mucous membranes, and internal organs.

How Fluconazole Works in the Body

Fluconazole is a triazole antifungal that interferes with the synthesis of ergosterol, an essential component of fungal cell membranes. By inhibiting the fungal enzyme lanosterol 14α-demethylase (a cytochrome P450 isozyme), the drug prevents conversion of lanosterol to ergosterol. This disruption weakens the cell membrane, leading to increased permeability and ultimately halting fungal growth. Oral fluconazole is well absorbed, reaching peak plasma concentrations within 1-2 hours. It distributes widely, including into cerebrospinal fluid, making it useful for central nervous system fungal infections.

Conditions Treated by Fluconazole

Fluconazole is approved for several indications, primarily based on regulatory assessments in the United States, European Union, and Hong Kong. The most common approved uses include:

  • Vulvovaginal candidiasis - short-course oral therapy (single 150 mg dose or 3-day regimen).
  • Oropharyngeal and esophageal candidiasis - usually 200 mg on day 1 followed by 100 mg daily.
  • Candidemia and other systemic candidiasis - loading dose of 400 mg on day 1, then 200-400 mg daily depending on severity.
  • Cryptococcal meningitis (induction phase) - high-dose 400 mg daily for at least two weeks, followed by maintenance dosing.
  • Prevention of fungal infections in immunocompromised patients (e.g., bone-marrow transplant recipients) - prophylactic dosing typically 200 mg three times weekly.

These indications are supported by clinical trials and guideline recommendations from bodies such as the Infectious Diseases Society of America (IDSA) and local Hong Kong health authorities.

Evidence-Based Off-Label Uses

Some clinicians use fluoro­conazole for conditions that are not formally approved but have supporting evidence:

  • Prophylaxis for patients with neutropenia - several randomized studies show reduced incidence of invasive candidiasis when 400 mg weekly is given.
  • Treatment of dermatophyte infections (e.g., tinea corporis) - limited case series suggest effectiveness, though topical agents remain first-line.
  • Recurrent vulvovaginal candidiasis - extended low-dose regimens (e.g., 100 mg weekly) have demonstrated reduced recurrence rates in controlled trials.

Disclaimer: Off-label use of fluoro­conazole requires supervision by a qualified healthcare professional. Decisions should be individualized based on risk-benefit assessment.

Who Should Not Use Fluconazole?

Absolute contraindications

  • Known hypersensitivity to fluoro­conazole or any other triazole antifungal.
  • Concurrent use of terfenadine or cisapride, medications that are contraindicated due to potential serious cardiac arrhythmias.

Relative contraindications

  • Severe liver impairment (Child-Pugh class C) - dose adjustment or alternative therapy may be needed.
  • Pregnancy (Category D) - fluoro­conazole crosses the placenta and is associated with fetal abnormalities in animal studies; it should be avoided unless the benefit outweighs the risk.
  • Breastfeeding - small amounts are excreted in breast milk; caution is advised.

Special populations

  • Elderly patients - may have reduced hepatic clearance; monitor for toxicity.
  • Renal impairment - because fluoro­conazole is largely excreted unchanged, dose reduction is recommended when creatinine clearance is < 50 mL/min.
  • Patients with cardiac disease - consider baseline QT interval assessment, as fluoro­conazole can prolong QT in susceptible individuals.

Safety Profile and Interactions

Common Side Effects

  • Nausea, abdominal discomfort, and mild headache - usually transient and do not require intervention.
  • Elevated liver enzymes - routine monitoring is advised for prolonged therapy.
  • Skin rash - benign in most cases, but discontinue if rash becomes severe.

Serious Adverse Events

  • Hepatotoxicity - rare but can be severe; stop the drug and assess liver function if jaundice or marked transaminase rise occurs.
  • Severe allergic reactions (e.g., Stevens-Johnson syndrome) - requires immediate medical attention.
  • QT prolongation leading to torsades de pointes - reported in patients with pre-existing cardiac risk factors.

Drug Interactions

  • Major: Concomitant use with cisapride, terfenadine, or pimozide can cause life-threatening arrhythmias.
  • Moderate: Drugs metabolized by CYP2C9 (e.g., warfarin) may have increased plasma levels; INR should be monitored.
  • Moderate: Phenytoin, carbamazepine, and rifampin can reduce fluoro­conazole concentrations, potentially lowering efficacy.
  • Moderate: Oral contraceptives - fluoro­conazole may increase hormone levels; additional non-hormonal contraception is advised.

Food and Lifestyle Interactions

  • Fluoro­conazole can be taken with or without food; taking it with a meal may reduce gastrointestinal upset.
  • Alcohol does not have a direct interaction, but excessive intake can exacerbate liver toxicity.
  • Patients should avoid driving or operating heavy machinery if they experience dizziness or visual disturbances.

If specific interaction data for a particular medication is limited, patients should always inform their healthcare provider of all concurrent drugs, supplements, and herbal products.

How to Take Fluconazole

  • Standard dosing begins with the strength appropriate for the diagnosed infection (e.g., a single 150 mg pill for uncomplicated vaginal candidiasis).
  • Maintenance dosing for chronic conditions often involves 100 mg to 200 mg daily or weekly, depending on the protocol.
  • Renal adjustment: For creatinine clearance < 50 mL/min, the usual recommendation is 50-100 mg every 48 hours or as directed by a clinician.
  • Hepatic impairment: Start with the lowest effective dose and monitor liver enzymes regularly.
  • Administration: Swallow the pill whole with a glass of water. No crushing or chewing is required.
  • Missed dose: Take the missed dose as soon as remembered unless it is almost time for the next scheduled dose; do not double the dose.
  • Overdose: Symptoms may include severe nausea, vomiting, abdominal pain, and altered mental status. Seek emergency medical care; supportive measures and gastrointestinal decontamination are the primary treatments.
  • Discontinuation: Some infections (e.g., cryptococcal meningitis) require a gradual taper to prevent relapse; abrupt cessation without medical advice is discouraged.

Monitoring and Follow-Up

  • Liver function tests (LFTs) are recommended before initiating therapy and periodically during prolonged treatment.
  • Renal function should be assessed in patients with known kidney disease, especially when high doses are used.
  • Therapeutic drug monitoring is not routinely required for fluoro­conazole but may be considered in severe infections or when interacting drugs affect its levels.
  • Patients should report symptoms such as persistent nausea, jaundice, dark urine, or unusual cardiac palpitations promptly.

Storage and Handling

  • Store fluoro­conazole tablets at room temperature (20-25 °C), away from excess moisture and direct sunlight.
  • Keep the medication out of reach of children and pets.
  • Do not use tablets that are discolored, cracked, or past the expiration date indicated on the package.
  • Dispose of unused pills according to local pharmacy take-back programs or follow the disposal instructions on the label.

Medication-Specific Glossary

Lanosterol 14α-demethylase
The fungal enzyme inhibited by fluoro­conazole, essential for converting lanosterol to ergosterol in cell membranes.
Therapeutic drug monitoring
Measurement of drug concentrations in blood to ensure efficacy while avoiding toxicity; occasionally used for fluoro­conazole in complex cases.
QT prolongation
Extension of the heart’s electrical repolarization period, which can predispose to dangerous arrhythmias; fluoro­conazole may cause this in susceptible patients.
CYP2C9 inhibition
Fluoro­conazole can reduce the activity of this liver enzyme, leading to higher levels of drugs metabolized by CYP2C9 (e.g., warfarin).

Medical Disclaimer

This article provides educational information about fluoro­conazole and is not a substitute for professional medical advice. Treatment decisions, including use for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

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